Levetiracetam Canon
Levetiracetam Canon: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Levetiracetam Canon
ATX code: N03AX14
Active ingredient: Levetiracetam (Levetiracetam)
Producer: Kanonpharma Production, CJSC (Russia)
Description and photo updated: 30.11.2018
Prices in pharmacies: from 295 rubles.
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Levetiracetam Canon is an antiepileptic drug.
Release form and composition
Dosage form - film-coated tablets: round (at a dosage of 250 mg) or oval (at a dosage of 500 and 1000 mg), biconvex, with a risk, a blue film shell, an almost white core in a cross section (250 mg tablets - by 10 pcs.in blister contour packs, in a cardboard bundle 1, 3 or 6 packages; 15 pcs. In blister contour packs, in a cardboard bundle 2 or 4 packs; tablets 500 and 1000 mg - 10 pcs. In blister contour packs, in a cardboard box of 1, 3 or 6 packs; each pack also contains instructions for the use of Levetiracetam Canon).
Composition of 1 tablet:
- active substance: levetiracetam - 250, 500 or 1000 mg;
- auxiliary components: microcrystalline cellulose, croscarmellose sodium, mannitol, calcium stearate, colloidal silicon dioxide, povidone;
- film casing: Opadray II blue [titanium dioxide, macrogol (polyethylene glycol), talc, polyvinyl alcohol, aluminum varnish based on charming red dye, aluminum varnish based on indigo carmine dye].
Pharmacological properties
Pharmacodynamics
The active ingredient of Levetiracetam Canon is levetiracetam, a pyrrolidone derivative (S-enantiomer of α-ethyl-2-oxo-1-pyrrolidine-acetamide), which is not similar in chemical structure to traditional antiepileptic drugs. The mechanism of its action is not fully understood, but it has been precisely established that it differs from the mechanisms of action of known antiepileptic drugs. In experiments in vivo and in vitro, it was found that levetiracetam does not affect the basic characteristics of cells and normal transmission. In vitro experiments have shown the effect of the drug on the intraneuronal concentration of calcium ions due to partial inhibition of the current of calcium ions through the N-type channels and a decrease in the release of calcium from intraneuronal stores. Levetiracetam also partially restores currents through glycine-dependent channels,as well as ion channels of GABA (gamma-aminobutyric acid) receptors.
One of the putative mechanisms of action of the drug is the proven binding of the SV2A synaptic vesicles to the glycoprotein, which is found in the gray matter of the spinal cord and brain. It is believed that in this way an anticonvulsant effect occurs, which is manifested by counteracting the hypersynchronization of neural activity. In addition, levetiracetam acts on glycine receptors and GABA receptors, modulating them through various endogenous agents.
Levetiracetam Canon does not affect normal neurotransmission, but suppresses the excitation of glutamate receptors and epileptiform neuronal outbreaks caused by the GABA agonist bikuculin.
It has been established that levetiracetam is active against both focal and generalized epileptic seizures [photoparoxysmal reaction (FPR) or epileptiform manifestations].
Pharmacokinetics
Levetiracetam is completely absorbed from the gastrointestinal tract. It dissolves well in water, penetrates into tissues and liquids. Absorption is linear, so the plasma concentration of the drug can be predicted depending on the dose used, expressed in mg / kg body weight. The dose and timing of meals do not affect the extent of absorption.
Levetiracetam is characterized by a very high bioavailability - approximately 100%.
The maximum plasma concentration (Cmax) after taking a dose of 100 mg is achieved within 1.3 hours and is 31 μg / ml with a single dose, 43 μg / ml - with multiple doses (2 times a day). Equilibrium concentration is observed after two days when using Levetiracetam Canon 2 times a day.
In children, the pharmacokinetics of levetiracetam is linear in the range of daily doses from 20 to 60 mg / kg. Cmax is reached within 0.5-1 hours.
Levetiracetam and its main metabolite bind to plasma proteins by no more than 10%. The volume of distribution (Vd) is approximately 0.5–0.7 l / kg.
It is metabolized mainly by enzymatic hydrolysis of the acetamide group. The primary pharmacologically inactive metabolite (ucb L057) is formed without the participation of liver cytochrome P 450.
Levetiracetam Canon does not affect the enzymatic activity of hepatocytes.
In vitro studies have not shown inhibition of the main forms of cytochrome P 450 (CYP 3A4, 1A2, 2D6, 2C19, 2E1, 2C9, 2A6) by levetiracetam and its main metabolite, as well as the activity of epoxide hydroxylase and glucuronyl transferase (UGT1A1, UGT1A6). In addition, according to in vitro studies, it was found that levetiracetam does not affect the glucuronidation of valproic acid.
The half-life (T 1/2) from the blood plasma of an adult patient is 7 ± 1 h, and does not depend on the dosage regimen and the method of administration of the drug. However, it increases to 10-11 hours in elderly patients, which is associated with age-related functional impairment of the kidneys.
The total clearance averages 0.96 ml / min / kg. It is excreted mainly by the kidneys (95%). The renal clearance of levetiracetam and its metabolite is 0.6 and 4.2 ml / min / kg, respectively.
In case of impaired renal function, the clearance of levetiracetam and its primary metabolite correlates with creatinine clearance (CC), and therefore, CC should be taken into account when selecting the optimal dose. In adult patients with end-stage renal failure, T 1/2 is 25 hours between dialysis sessions, 3.1 hours during dialysis. During a 4-hour dialysis session, up to 51% of the drug is excreted from the body.
In mild and moderate liver functional disorders, significant changes in the clearance of levetiracetam are not observed. In most patients with severe hepatic impairment and concomitant renal failure, the clearance of levetiracetam decreases by more than 50%.
In children, T 1/2 after a single dose of 20 mg / kg is 5-6 hours. The total clearance is in direct proportion to body weight and is approximately 40% higher than in adults.
Indications for use
As monotherapy, Levetiracetam Canon is used for partial seizures (including secondary generalization) in the case of newly diagnosed epilepsy in adults and adolescents from 16 years of age.
As part of complex therapy, the drug is prescribed for the following diseases / conditions:
- primary generalized convulsive (tonic-clonic) seizures in idiopathic generalized epilepsy in adults and adolescents over 12 years old;
- myoclonic seizures in juvenile myoclonic epilepsy in adults and adolescents over 12 years old;
- partial seizures (including those with secondary generalization) with epilepsy in adults and children from 6 years of age.
Contraindications
Absolute:
- period of breastfeeding;
- body weight less than 20 kg;
- children under 6 years of age - with partial seizures against the background of epilepsy;
- children under 12 years of age - with myoclonic seizures against the background of juvenile myoclonic epilepsy, as well as with primary generalized convulsive (tonic-clonic) seizures against the background of idiopathic generalized epilepsy;
- children under 16 years of age - with partial seizures against the background of newly diagnosed epilepsy;
- hypersensitivity to any component of the drug or other pyrrolidone derivatives.
Relative (Levetiracetam Canon tablets are used with caution, after assessing the benefit / risk ratio):
- renal failure (CC less than 50 ml / min);
- liver disease in the stage of decompensation;
- depression, suicidal behavior;
- advanced age (over 65);
- simultaneous use of sulfonamides, non-steroidal anti-inflammatory drugs, methotrexate, probenecid.
Levetiracetam Canon, instructions for use: method and dosage
Levetiracetam Canon tablets are taken orally, swallowed whole and washed down with a sufficient amount of water. Meal time does not matter.
Monotherapy
As a monopreparation for adults and adolescents from 16 years of age, Levetiracetam Canon is prescribed in an initial dose of 250 mg 2 times a day.
If necessary, after 2 weeks, the dose is increased to 500 mg 2 times a day. If the effect is not enough, it continues to increase, up to the maximum allowable daily dose of 3000 mg, divided into 2 doses of 1500 mg.
Complex therapy
Adults and adolescents from 16 years old with a body weight of more than 50 kg at the beginning of treatment are prescribed 500 mg 2 times a day. If the effect is insufficient, but provided that the drug is well tolerated, the dose is increased to a maximum daily dose of 3000 mg in 2 divided doses. The dose is increased at intervals of 2-4 weeks by 500 mg 2 times a day.
Treatment of children over 6 years old begins with a daily dose of 20 mg / kg in 2 divided doses. If necessary, the daily dose continues to be increased by 20 mg / kg at intervals of 2 weeks, up to the maximum allowable dose of 60 mg / kg / day (in 2 divided doses). In case of poor tolerance of the drug, the dose is reduced. Levetiracetam Canon is recommended for children to be prescribed in the minimum effective dose.
For children under 16 years of age weighing more than 50 kg, the drug is dosed as for adults.
Special patient groups
In renal failure, the dose of Levetiracetam Canon is adjusted depending on the QC.
In men, CC can be calculated based on the serum creatinine concentration using the following formula:
CC (ml / min) = (140 - age) × body weight (kg) / 72 × serum CC (mg / dl).
In women, CC is determined by multiplying the value obtained according to the described formula by a factor of 0.85.
Recommended doses of Canon Levetiracetam for adults:
- CC 50–79 ml / min: 500–1000 mg 2 times a day;
- CC 30–49 ml / min: 250–750 mg 2 times a day;
- CC <30 ml / min: 250-500 mg 2 times a day;
- dialysis: on the first day of treatment - 750 mg, then - 500–1000 mg once a day + an additional dose of 250–500 mg after dialysis.
Recommended doses of Canon Levetiracetam for children:
- CC 50–79 ml / min: 10–20 mg / kg per day;
- CC 30–49 ml / min: 5–15 mg / kg per day;
- CC <30 ml / min: 5-10 mg / kg per day;
- dialysis: on the first day of treatment - 15 mg / kg, then - 10–20 mg / kg once a day + an additional dose of 5–10 mg / kg after dialysis.
For mild to moderate liver dysfunction, dose adjustment is not required. In patients with decompensated hepatic impairment and renal insufficiency with CC <60 ml / min, it is recommended to reduce the daily dose by 50%.
Side effects
Possible side effects (according to the frequency of development, they are classified as follows: very often -> 10% of cases, often -> 1% and 0.1% and 0.01% and <0.1%, very rarely - <0.01%):
- from the nervous system and psyche: very often - headache, drowsiness, asthenic syndrome; often - mood swings, agitation, dizziness, irritability, nervousness, depression, imbalance, insomnia, anxiety, impaired thinking, vertigo, tremors, personality disorders, hostility / aggressiveness, seizures; infrequently - behavioral disorders, memory impairment, amnesia, confusion, decreased concentration, hallucinations, emotional lability, psychotic disorders, ataxia, suicidal intentions, attempts at suicide; rarely - impaired thinking, personality disorder, hyperkinesia, dyskinesia, choreoathetosis, suicide;
- from the digestive system: often - nausea, abdominal pain, vomiting, anorexia, dyspepsia, diarrhea, increased body weight; infrequently - changes in liver function tests, pancreatitis; rarely - weight loss, hepatitis, liver failure;
- from the respiratory system: often - increased cough;
- on the part of the organs of vision: infrequently - violation of accommodation, diplopia;
- on the part of the skin: often - skin rash, infrequently - itching, eczema, alopecia (in some cases, after the cancellation of Levetiracetam Canon, hair restoration was observed); rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis;
- laboratory data: infrequently - leukopenia, thrombocytopenia; rarely - neutropenia, pancytopenia (sometimes with depression of bone marrow function);
- others: muscle weakness, myalgia, a tendency to injury, nasopharyngitis, infections.
In children, the following disorders are possible: behavioral disorders, emotional lability, mood swings, aggressiveness, agitation, lethargy, vomiting.
Overdose
Symptoms of levetiracetam overdose are aggressiveness, agitation, drowsiness, depression of consciousness, coma, respiratory depression.
In the acute period, induce vomiting, rinse the stomach, take activated charcoal. The specific antidote for the substance is unknown. Treatment is symptomatic, carried out in a hospital. To remove the drug from the body, hemodialysis is used (the effectiveness of dialysis to remove levetiracetam is 60%, its primary metabolite is 74%).
special instructions
In the presence of kidney disease and decompensated liver disease, it is recommended to conduct an examination of renal function before starting treatment. If this is due to the patient's condition, the therapeutic scheme is corrected.
There are reports of cases of suicidal intentions and attempts, therefore, patients should be informed about the need to consult a doctor if any signs of developing depression or suicidal intentions appear.
When transferring a patient to Levetiracetam Canon, other antiepileptic drugs are recommended to be canceled gradually.
Levetiracetam Canon cannot be canceled suddenly. If treatment should be interrupted, a single dose should be gradually reduced: for adults - by 500 mg every 2–4 weeks, for children - no more than 10 mg / kg every 2 weeks.
Influence on the ability to drive vehicles and complex mechanisms
The effect of the drug on human cognitive and psychomotor functions has not been studied. However, given the likelihood of developing reactions from the central nervous system, during treatment it is worth refusing to drive a car and perform potentially dangerous work that requires speed of reactions and increased attention.
Application during pregnancy and lactation
Adequate and carefully controlled studies on the effect of levetiracetam on the course of pregnancy have not been conducted, therefore, during the period of gestation, Levetiracetam Canon can be used only in exceptional cases, when the expected benefit definitely outweighs all possible risks.
Physiological changes in the female body during pregnancy can affect the plasma concentration of levetiracetam. A decrease in its level is usually noted, especially in the third trimester (up to 60% of the baseline concentration observed before pregnancy).
If Levetiracetam Canon is used during pregnancy, the woman should be under special medical supervision. In this case, one should take into account the deterioration in the course of the disease, which can cause a break in antiepileptic therapy, which is fraught with negative consequences for both the mother and the fetus.
Women of reproductive age need to use reliable methods of contraception during therapy.
The drug passes into the mother's milk. If treatment is necessary during lactation, breastfeeding should be abandoned.
Pediatric use
Age restrictions (the drug should not be used for the treatment of patients under the specified age):
- partial seizures against the background of epilepsy - up to 6 years;
- myoclonic seizures against the background of juvenile myoclonic epilepsy, as well as primary generalized convulsive (tonic-clonic) seizures against the background of idiopathic generalized epilepsy - up to 12 years;
- partial seizures in newly diagnosed epilepsy - up to 16 years.
The available data on the use of Levetiracetam Canon in children does not indicate its negative effect on development and puberty. However, until now, the long-term effects of the effect of therapy on the functions of the endocrine glands, growth, sexual development, fertility, intellectual development, and the ability to learn are unknown.
With impaired renal function
Levetiracetam Canon should be used with caution in renal insufficiency with CC less than 50 ml / min. Correction of dosage regimen is required.
For violations of liver function
Levetiracetam Canon should be used with caution in the treatment of patients with liver disease in the stage of decompensation. Correction of dosage regimen is required.
Use in the elderly
Levetiracetam Canon is used with caution when treating patients over the age of 65.
Drug interactions
Levetiracetam does not interact with antiepileptic drugs such as phenobarbital, valproic acid, gabapentin, lamotrigine, carbamazepine, phenytoin, primidone.
Levetiracetam in a daily dose of 1000 mg does not affect the pharmacokinetic parameters of oral contraceptives - levonorgestrel and ethinyl estradiol, in a daily dose of 2000 mg does not change the pharmacokinetics of warfarin and digoxin. These drugs do not alter the pharmacokinetics of levetiracetam.
With the simultaneous use of topiramate, the risk of developing anorexia increases.
In children taking anticonvulsants, which are inducers of microsomal oxidation in the liver, the clearance of levetiracetam is 20% higher than in children who are not receiving microsomal oxidation inducers. In the case of simultaneous use of probenecid at a dose of 500 mg 4 times a day, a decrease in renal secretion of the primary metabolite of levetiracetam was observed.
There are no data on interactions with alcohol.
Analogs
Analogues of Levetiracetam Canon are Algerica, Benzonal, Valparin, Gabapentin, Zenitetam, Zonegran, Carbamazepine, Keppra, Konvulex, Lamictal, Lyrica, Neurontin, Pregabalin, Seizar, Tegretol, Topamax, Faykompil and others.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C in a dry, dark place.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Levetiracetam Canon
Reviews about Levetiracetam Canon are mostly positive: the drug effectively prevents seizures. Patients report a significantly better tolerance of levetiracetam compared to valproic acid.
Negative messages contain complaints about the development of adverse reactions, the most common of which are drowsiness, weakness, and dizziness.
Price for Levetiracetam Canon in pharmacies
Approximate prices for Canon Levetiracetam (for a pack of 30 tablets):
- dosage 250 mg - 239-345 rubles;
- dosage of 500 mg - 480-610 rubles;
- dosage 1000 mg - 885-1180 rubles.
Levetiracetam Canon: prices in online pharmacies
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Drug name Price Pharmacy |
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Levetiracetam Canon 250 mg film-coated tablets 30 pcs. 295 RUB Buy |
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Levetiracetam Canon 500 mg film-coated tablets 30 pcs. RUB 538 Buy |
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Levetiracetam Canon 1000 mg film-coated tablets 30 pcs. RUB 960 Buy |
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Levetiracetam Canon 500 mg film-coated tablets 60 pcs. 997 RUB Buy |
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Levetiracetam Canon tablets p.o. 1000mg 30 pcs. 1199 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
